scholarly journals Quaternary Ammonium Chitosans: The Importance of the Positive Fixed Charge of the Drug Delivery Systems

2020 ◽  
Vol 21 (18) ◽  
pp. 6617 ◽  
Author(s):  
Angela Fabiano ◽  
Denise Beconcini ◽  
Chiara Migone ◽  
Anna Maria Piras ◽  
Ylenia Zambito
Keyword(s):  
Drug Delivery ◽  
Quaternary Ammonium ◽  
Drug Delivery Systems ◽  
Ex Vivo ◽  
Delivery Systems ◽  
Fixed Charge ◽  
Innovative Drug ◽  
Natural Polysaccharide ◽  
The Impact

As a natural polysaccharide, chitosan has good biocompatibility, biodegradability and biosecurity. The hydroxyl and amino groups present in its structure make it an extremely versatile and chemically modifiable material. In recent years, various synthetic strategies have been used to modify chitosan, mainly to solve the problem of its insolubility in neutral physiological fluids. Thus, derivatives with negative or positive fixed charge were synthesized and used to prepare innovative drug delivery systems. Positively charged conjugates showed improved properties compared to unmodified chitosan. In this review the main quaternary ammonium derivatives of chitosan will be considered, their preparation and their applications will be described to evaluate the impact of the positive fixed charge on the improvement of the properties of the drug delivery systems based on these polymers. Furthermore, the performances of the proposed systems resulting from in vitro and ex vivo experiments will be taken into consideration, with particular attention to cytotoxicity of systems, and their ability to promote drug absorption.

scholarly journals Polymer-Based Smart Drug Delivery Systems for Skin Application and Demonstration of Stimuli-Responsiveness

Polymers ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1285
Author(s):  
Louise Van Gheluwe ◽  
Igor Chourpa ◽  
Coline Gaigne ◽  
Emilie Munnier
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Ex Vivo ◽  
Delivery Systems ◽  
Stimuli Responsive ◽  
Stimuli Responsive Polymers ◽  
Smart Drug ◽  
Smart Drug Delivery

Progress in recent years in the field of stimuli-responsive polymers, whose properties change depending on the intensity of a signal, permitted an increase in smart drug delivery systems (SDDS). SDDS have attracted the attention of the scientific community because they can help meet two current challenges of the pharmaceutical industry: targeted drug delivery and personalized medicine. Controlled release of the active ingredient can be achieved through various stimuli, among which are temperature, pH, redox potential or even enzymes. SDDS, hitherto explored mainly in oncology, are now developed in the fields of dermatology and cosmetics. They are mostly hydrogels or nanosystems, and the most-used stimuli are pH and temperature. This review offers an overview of polymer-based SDDS developed to trigger the release of active ingredients intended to treat skin conditions or pathologies. The methods used to attest to stimuli-responsiveness in vitro, ex vivo and in vivo are discussed.

Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) Containing Rice Bran Oil for Enhanced Fenofibrate Oral Delivery: In Vitro Digestion, Ex Vivo Permeability, and In Vivo Bioavailability Studies

2020 ◽  
Vol 21 (6) ◽  
Author(s):  
Christina Karavasili ◽  
Ioannis I. Andreadis ◽  
Maria P. Tsantarliotou ◽  
Ioannis A. Taitzoglou ◽  
Paschalina Chatzopoulou ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Rice Bran ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Rice Bran Oil ◽  
Ex Vivo ◽  
In Vitro Digestion ◽  
Delivery Systems

scholarly journals Ex Vivo and In Vivo Characterization of Interpolymeric Blend/Nanoenabled Gastroretentive Levodopa Delivery Systems

2017 ◽  
Vol 2017 ◽  
pp. 1-14 ◽  
Author(s):  
Ndidi C. Ngwuluka ◽  
Yahya E. Choonara ◽  
Girish Modi ◽  
Lisa C. du Toit ◽  
Pradeep Kumar ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Ex Vivo ◽  
Delivery Systems ◽  
Pharmacokinetic Parameters ◽  
Gastric Residence Time ◽  
Systemic Bioavailability ◽  
Absorption Window

One approach for delivery of narrow absorption window drugs is to formulate gastroretentive drug delivery systems. This study was undertaken to provide insight into in vivo performances of two gastroretentive systems (PXLNETand IPB matrices) in comparison to Madopar® HBS capsules. The pig model was used to assess gastric residence time and pharmacokinetic parameters using blood, cerebrospinal fluid (CSF), and urine samples. Histopathology and cytotoxicity testing were also undertaken. The pharmacokinetic parameters indicated that levodopa was liberated from the drug delivery systems, absorbed, widely distributed, metabolized, and excreted.Cmaxwere 372.37, 257.02, and 461.28 ng/mL and MRT were 15.36, 14.98, and 13.30 for Madopar HBS capsules,PXLNET, and IPB, respectively. In addition, X-ray imaging indicated that the gastroretentive systems have the potential to reside in the stomach for 7 hours. There was strong in vitro-in vivo correlation for all formulations withr2values of 0.906, 0.935, and 0.945 for Madopar HBS capsules,PXLNET, and IPB, respectively. Consequently,PXLNETand IPB matrices have pertinent potential as gastroretentive systems for narrow absorption window drugs (e.g., L-dopa) and, in this application specifically, enhanced the central nervous system and/or systemic bioavailability of such drugs.

scholarly journals Tuning the properties of pH responsive nanoparticles to control cellular interactions in vitro and ex vivo

2016 ◽  
Vol 7 (38) ◽  
pp. 6015-6024 ◽  
Author(s):  
S. K. Mann ◽  
A. Dufour ◽  
J. J. Glass ◽  
R. De Rose ◽  
S. J. Kent ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Human Blood ◽  
Drug Delivery Systems ◽  
Cultured Cells ◽  
Ex Vivo ◽  
Delivery Systems ◽  
Effective Drug ◽  
Cellular Interactions ◽  
Ph Responsive

Engineering the properties of nanoparticles to limit non-specific cellular interactions is critical for developing effective drug delivery systems. Differences between interactions with cultured cells and human blood highlights the need for appropriate assays.

scholarly journals DELOS Nanovesicles-Based Hydrogels: An Advanced Formulation for Topical Use

Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 199
Author(s):  
Lídia Ballell-Hosa ◽  
Elisabet González-Mira ◽  
Hector Santana ◽  
Judit Morla-Folch ◽  
Marc Moreno-Masip ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Resonance Energy Transfer ◽  
Resonance Energy ◽  
Colloidal Dispersions ◽  
Delivery Systems ◽  
Innovative Drug ◽  
Liquid Form ◽  
Recent Developments

Topical delivery has received great attention due to its localized drug delivery, its patient compliance, and its low risk for side effects. Recent developments have focused on studying new drug delivery systems as a strategy for addressing the challenges of current topical treatments. Here we describe the advances on an innovative drug delivery platform called DELOS nanovesicles for topical drug delivery. Previously, the production of DELOS nanovesicles demonstrated potentiality for the topical treatment of complex wounds, achieving well-tolerated liquid dispersions by this route. Here, research efforts have been focused on designing these nanocarriers with the best skin tolerability to be applied even to damaged skin, and on exploring the feasibility of adapting the colloidal dispersions to a more suitable dosage form for topical application. Accordingly, these drug delivery systems have been efficiently evolved to a hydrogel using MethocelTM K4M, presenting proper stability and rheological properties. Further, the integrity of these nanocarriers when being gellified has been confirmed by cryo-transmission electron microscopy and by Förster resonance energy transfer analysis with fluorescent-labeled DELOS nanovesicles, which is a crucial characterization not widely reported in the literature. Additionally, in vitro experiments have shown that recombinant human Epidermal Growth Factor (rhEGF) protein integrated into gellified DELOS nanovesicles exhibits an enhanced bioactivity compared to the liquid form. Therefore, these studies suggest that such a drug delivery system is maintained unaltered when hydrogellified, becoming the DELOS nanovesicles-based hydrogels, an advanced formulation for topical use.

scholarly journals Evaluation of Experimental Multi-Particulate Polymer-Coated Drug Delivery Systems with Meloxicam

Coatings ◽  
2020 ◽  
Vol 10 (5) ◽  
pp. 490
Author(s):  
Mircea Hîrjău ◽  
Dalia Simona Miron ◽  
Valentina Anuța ◽  
Dumitru Lupuliasa ◽  
Mihaela Violeta Ghica ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery Systems ◽  
In Vitro Release ◽  
Spray Coating ◽  
Delivery Systems ◽  
Experimental Systems ◽  
The Impact ◽  
Vitro Release

The objectives of this study are the development and evaluation of modified release multi-particulate drug delivery systems containing a BCS class II drug (meloxicam), formulated as polymer-coated pellets. Inert seeds containing microcrystalline cellulose, lactose monohydrate, and polyvinylpyrrolidone were prepared by extrusion-spheronization. The obtained cores were loaded with meloxicam using the drug layering technique, by spray coating in a fluidized bed with a liquid dispersion of the drug. The resulting drug pellets were film-coated with various polymers (Acryl-EZE® 93O, Eudragit® RS 30-D as well as experimental composite obtained by adding Methocel™ E5 Premium LV as pore forming agent to the extended release polymer Eudragit® RS 30-D). All experimental systems were evaluated by scanning electron microscopy and in vitro release testing, in an attempt to investigate the characteristics of the film coatings and their influence on drug release from the multi-particulate systems. The in vitro release study was performed in two stages, using two media with pH values corresponding to the gastric and intestinal environment (HCl 0.1N, pH = 1.2 for the first two hours of the test and phosphate buffer 50 mM, pH 6.8 for the next 4 h). The in vitro release data have highlighted the impact of the formulation factors on the drug release.

Lipid Digestion as a Trigger for Supersaturation: Evaluation of the Impact of Supersaturation Stabilization on the in Vitro and in Vivo Performance of Self-Emulsifying Drug Delivery Systems

2012 ◽  
Vol 9 (7) ◽  
pp. 2063-2079 ◽  
Author(s):  
Mette U. Anby ◽  
Hywel D. Williams ◽  
Michelle McIntosh ◽  
Hassan Benameur ◽  
Glenn A. Edwards ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Lipid Digestion ◽  
The Impact
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